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TGF-beta/Smad

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Cat. No. Product Name Field of Application Chemical Structure
DC8020 A77-01 Featured A 77-01 is a potent inhibitor of TGF-β type I receptor superfamily activin-like kinase ALK5 with IC50 of 25 nM.
DC11778 PKC-IN-6c A novel, potent, brain permeant PKC inhibitor with IC50 of 80 nM, without detectable binding to the estrogen receptor (Ki>10 uM).
DC7286 A83-01 Featured A83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively).
DC10052 Bisindolylmaleimide X(Ro 31-8425) Featured Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC).
DC8504 Bisindolylmaleimide X HCl Featured Bisindolylmaleimide X is a cell-permeable, reversible, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 15 nM, rat brain PKC).
DC11038 Bryostatin 1 Featured Bryostatin 1 (NSC 339555) is a macrocyclic lactone derived from a marine invertebrate, fuctions as an activator of PKC with high binding affinity (Ki=1.35 nM).
DC7643 DMH1 Featured DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR.
DC5057 Enzastaurin (LY317615) Featured Enzastaurin (LY317615) is a potent PKCβ selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Phase 3.
DC8342 EW-7197 Featured EW-7197 is a potent ALK5 inhibitor. EW-7197 showed potent in vivo anti-metastatic activity, indicating its potential for use as an anti-cancer therapy.
DC7132 GF 109203X Featured GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.
DC7660 Go 6983 Featured Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.
DC7980 GW-6604 Featured GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity.
DC7146 GW788388 Featured GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.
DC7835 H-89 2HCl Featured H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II.
DC10983 ICA-1(ICA-1T) Featured ICA-1(ICA-1T)is a potent, specific inhibitor of Protein Kinase C-iota (PKC-ι) with IC50 of 0.1 uM, does not inhibit PKC-ζ, the closely related atypical PKC family member.
DC8028 ITD-1 Featured ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.
DC7742 K02288 Featured K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
DC7914 LDN-214117 Featured LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
DC7189 LY-2109761 LY2109761 is a novel selective TGF-β receptor type I/II (TβRI/II) dual inhibitor with Ki of 38 nM and 300 nM, respectively; shown to negatively affect the phosphorylation of Smad2.
DC6306 LY2157299(Galunisertib) Featured LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.
DC10675 LY3200882 Featured LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.
DC8523 LY333531 Hydrochloride(Ruboxistaurin HCl) Featured LY-333,531 Hydrochloride is a potent, selective inhibitor of Protein Kinase C isozymes, PKC beta I (IC50 = 4.7 nM) and PKC beta II (IC50 = 5.9 nM). It is potentially beneficial for cancer research.
DC7587 ML347 Featured ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM
DC10645 Phorbol 12-myristate 13-acetate (PMA) Featured Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
DC7634 PKC-412 (Midostaurin) Featured PKC-412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.
DC8022 R-268712 Featured Potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 = 2.5 nM). Exhibits ~ 5000-fold selectivity over p38 MAPK. Suppresses development of renal fibrosis in a unilateral ureteral obstruction model. Also reduces proteinuria, glomeruloscler
DC7259 Repsox(ALK5 Inhibitor II) Featured RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.
DC7270 Ro 31-8220 mesylate Featured Ro 31-8220 mesylate (Bisindolylmaleimide IX) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.
DC5189 SB-431542 Featured SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
DC6312 SB525334 Featured SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
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